Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: The invention provides 1,4-dihydropyridine derivatives of formula (I) wherein R1 is optionally substituted C6-24aryl group or 5 to 6 membered heteroaryl group comprising 1 to 3 nitrogen atoms or other heteroatoms like oxygen and sulphur, and combinations thereof; R2 and R3 are independently hydrogen or C1-6alkyl group; R4 and R5 are independently hydrogen, C1-6alkyl group optionally substituted with amino, mono- or di(C1-6alkyl)amino, or with 5 to 24 membered optionally fused heterocyclic ring attached by nitrogen and optionally comprising additional 1 to 3 N, O, S heteroatoms and optionally substituted with C1-6alkyl group or C1-6 alkoxy group; R6 is C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-6alkyl or arylC1-6alkyl group; and stereoisomers including enantiomers, diastereomers, racemic mixtures, mixture of enantiomers and combination thereof, as well as polymorphs, pharmaceutically acceptable salts, solvates, esters and prodrugs thereof for use in the therapeutic or prophylactic treatment of a disorder medi

Abstract: Analogs of CCK(1-8) having dissociated activity with respect to stimulating the contraction of the gall bladder and arresting the secretion of gastric acid. Various analogs also exhibit improved anticonvulsive potency. The peptides are characterized by the following formula:X--R.sub.0 --R.sub.1 --Tyr(Y)--R.sub.3 --R.sub.4 --Trp--R.sub.6 --R.sub.7 --R.sub.8 --NHQwherein X is H, Suc, Ac, Oxa, Mal, Glt, Prp, Prl or Acr; R.sub.0 is Gln, pGlu, Cys, Tyr, Tyr(OCH.sub.3), des--NH.sub.2 --Tyr or desR.sub.0 ; R.sub.1 is Asp, Tyr(OH or SE), Ser(OH or SE), Hyp(OH or SE), Thr(OH or SE), Cys, Tyr(OCH.sub.3) or desR.sub.1 ; Y is OH or SE; R.sub.3 is Met, Nva or Nle; R.sub.4 is Gly, D--Cys or D--Ala; R.sub.6 is Met, Nva or Nle; R.sub.7 is Asp, Ser(SE), Thr(SE) or Hyp(SE); R.sub.8 is Phe or Tyr(OCH.sub.3); and Q is lower alkyl, fluoro lower alkyl or hydrogen; provided that when R.sub.3 and R.sub.6 are Met and R.sub.7 is Asp then R.sub.4 is D--Ala. A pharmaceutically acceptable salt thereof may also be employed.

Abstract: A method for sulfating a hydroxy amino acid or a residue of such an amino acid in a peptide by reaction with a reagent which is a tertiaryammonium salt of acetylsulfuric acid having the formula:[CH.sub.3 COOSO.sub.3 ].sup.- [R].sup.+wherein R is triethylamine, ethyldiisopropylamine, pyridine, 4-methylmorpholine or 4-N,N-dimethylaminopyridine. The .alpha.-amino group and any other labile side chains present may be protected or may be left unprotected at the time the sulfation takes place.

Abstract: A process for the preparation of L-aspartyl-(O-sulfato-L-tyrosyl)-L-methionyl-glycyl-L-tryptophyl-L-methion yl-L-aspartyl-L-phenylalanine amide, which comprises treating the protected octapeptide amide of the general formula (II) ##STR1## wherein X is BOC, Cbz or Ddz,Y is O.sup.t Bu, OBzl or OH andW is O.sup.t Bu, OBzl or OH,in the presence of an ether with an excess of the complex compound of sulfur trioxide and a tertiary amine containing at least one alkyl group, converting the obtained sulfate ester of the protected octapeptide amide into an alkali metal salt and simultaneously removing the formyl group from the tryptophan unit by reacting the sulfate ester with an alkali metal hydroxide, and then splitting off the remaining protective groups by acidolysis.